Peringatan Keamanan

Patients experiencing an overdose may present with bradycardia, hypotension, cardiac failure, dizziness, hypoglycemia, fatigue, vomiting, bronchospasm and heart block.L7985 Treat overdose with general supportive measures including intravenous atropine for bradycardia, vasopressors and intravenous fluids for hypotension, isoproterenol infusion for heart block, digitalis glycosides and diuretics for congestive heart failure, bronchodilators for bronchospasm, and intravenous glucose for hypoglycemia.L7985

Nebivolol

DB04861

small molecule approved investigational

Deskripsi

Nebivolol is a racemic mixture of 2 enantiomers where one is a beta adrenergic antagonist and the other acts as a cardiac stimulant without beta adrenergic activity.A182579 Treatment with nebivolol leads to a greater decrease in systolic and diastolic blood pressure than atenolol, propranolol, or pindolol.A182579 Nebivolol and other beta blockers are generally not first line therapies as many patients are first treated with thiazide diuretics.A182594

Nebivolol was granted FDA approval on 17 December 2007.L7985

Struktur Molekul 2D

Berat 405.435
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) d-nebivolol has a half life of 12 hours in CYP2D6 extensive metabolizers and 19 hours in poor metabolizers.[A182615,L7985]
Volume Distribusi For a 20mg dose, d-nebivolol has an apparent volume of distribution of 10,290.81±3911.72L, l-nebivolol has an apparent volume of distribution of 8,066.66±4,055.50L, and both enantiomers together have a volume of distribution of 10,423.42±6796.50L.[A183008]
Klirens (Clearance) For a 20mg dose, the clearance of d-nebivolol is 1241.63±749.77L/h, l-nebivolol is 435.53±180.93L/h, and both enantiomers is 635.31±300.25L/h.[A183008]

Absorpsi

The absorption of nebivolol is not affected by food.L7985 Nebivolol has a Tmax of 1.5-4 hours.L7985 Bioavailability can range from 12-96% for extensive to poor CYP2D6 metabolizers.A183008,A183011 For a 20mg dose, d-nebivolol has a Cmax of 2.75±1.55ng/mL, l-nebivolol has a Cmax of 5.29±2.06ng/mL, both enantiomers have a Cmax of 8.02±3.47ng/mL, and nebivolol glucuronides have a Cmax of 68.34±44.68ng/mL.A183008 For a 20mg dose, d-nebivolol has an AUC of 13.78±15.27ng\*h/mL, l-nebivolol has an AUC of 27.72±15.32ng\*h/mL, both enantiomers have an AUC of 41.50±29.76ng\*h/mL, and nebivolol glucuronides have an AUC of 396.78±297.94ng\*h/mL.A183008

Metabolisme

Nebivolol is metabolized mainly by glucuronidation and CYP2D6 mediated hydroxylation.A2762,A182603 Metabolism involves n-dealkylation, hydroxylation, oxidation, and glucuronidation.A183011 Aromatic hydroxyl and acyclic oxide metabolites are active, while n-dealkylated and glucuronides are inactive.A183011

Rute Eliminasi

In extensive CYP2D6 metabolizers, 38% is eliminated in the urine and 44% in the feces.L7985 In poor CYP2D6 metabolizers, 67% is eliminated in the urine and 13% in the feces.L7985 <1% of a dose is excreted as the unmetabolized drug.A182615

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food.

Interaksi Obat

1419 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Nebivolol is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Nebivolol is combined with Levodopa.
Risperidone Nebivolol may increase the hypotensive activities of Risperidone.
Ceritinib Nebivolol may increase the bradycardic activities of Ceritinib.
Ivabradine Nebivolol may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Nebivolol.
Alfuzosin Alfuzosin may increase the hypotensive activities of Nebivolol.
Amifostine Nebivolol may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Nebivolol.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Nebivolol.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Nebivolol.
Obinutuzumab Nebivolol may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Nebivolol.
Rituximab Nebivolol may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Nebivolol.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Nebivolol.
Doxapram Doxapram may decrease the antihypertensive activities of Nebivolol.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Nebivolol.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Nebivolol.
Naratriptan Naratriptan may decrease the antihypertensive activities of Nebivolol.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Nebivolol.
Dopamine Dopamine may decrease the antihypertensive activities of Nebivolol.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Nebivolol.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Nebivolol.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Nebivolol.
Naluzotan Naluzotan may decrease the antihypertensive activities of Nebivolol.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Nebivolol.
Cinitapride Cinitapride may decrease the antihypertensive activities of Nebivolol.
Tyramine Tyramine may decrease the antihypertensive activities of Nebivolol.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Nebivolol.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Nebivolol.
Atipamezole Atipamezole may decrease the antihypertensive activities of Nebivolol.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Nebivolol.
Piclozotan Piclozotan may decrease the antihypertensive activities of Nebivolol.
Idazoxan Idazoxan may decrease the antihypertensive activities of Nebivolol.
Tramazoline Tramazoline may decrease the antihypertensive activities of Nebivolol.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Nebivolol.
Fenozolone Fenozolone may decrease the antihypertensive activities of Nebivolol.
Xenon Xenon may decrease the antihypertensive activities of Nebivolol.
Buflomedil Buflomedil may decrease the antihypertensive activities of Nebivolol.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Nebivolol.
Mefenorex Mefenorex may decrease the antihypertensive activities of Nebivolol.
5-methoxy-N,N-dimethyltryptamine 5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Nebivolol.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Nebivolol.
Solriamfetol Solriamfetol may decrease the antihypertensive activities of Nebivolol.
Isoflurane Isoflurane may decrease the antihypertensive activities of Nebivolol.
Propofol Propofol may decrease the antihypertensive activities of Nebivolol.
Remifentanil Remifentanil may decrease the antihypertensive activities of Nebivolol.
Desflurane Desflurane may decrease the antihypertensive activities of Nebivolol.
Dutasteride Dutasteride may decrease the antihypertensive activities of Nebivolol.
Eletriptan Eletriptan may decrease the antihypertensive activities of Nebivolol.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Nebivolol.
Buspirone Buspirone may decrease the antihypertensive activities of Nebivolol.
Sufentanil Sufentanil may decrease the antihypertensive activities of Nebivolol.
Alfentanil Alfentanil may decrease the antihypertensive activities of Nebivolol.
Fentanyl Fentanyl may decrease the antihypertensive activities of Nebivolol.
Almotriptan Almotriptan may decrease the antihypertensive activities of Nebivolol.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Nebivolol.
Halothane Halothane may decrease the antihypertensive activities of Nebivolol.
Finasteride Finasteride may decrease the antihypertensive activities of Nebivolol.
Sevoflurane Sevoflurane may decrease the antihypertensive activities of Nebivolol.
Yohimbine Yohimbine may decrease the antihypertensive activities of Nebivolol.
Solifenacin Solifenacin may decrease the antihypertensive activities of Nebivolol.
Flibanserin Flibanserin may decrease the antihypertensive activities of Nebivolol.
Cariprazine Cariprazine may decrease the antihypertensive activities of Nebivolol.
Mianserin Mianserin may decrease the antihypertensive activities of Nebivolol.
Lurasidone Lurasidone may decrease the antihypertensive activities of Nebivolol.
Siponimod Siponimod may decrease the antihypertensive activities of Nebivolol.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Nebivolol.
Naxitamab Naxitamab may decrease the antihypertensive activities of Nebivolol.
Cannabidiol The metabolism of Nebivolol can be decreased when combined with Cannabidiol.
Amiodarone The therapeutic efficacy of Nebivolol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Nebivolol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Nebivolol.
Disopyramide Disopyramide may increase the bradycardic activities of Nebivolol.
Dronedarone Dronedarone may increase the bradycardic activities of Nebivolol.
Fingolimod Nebivolol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Nebivolol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Nebivolol.
Methacholine Nebivolol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Nebivolol.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Nebivolol.
Propafenone The risk or severity of adverse effects can be increased when Propafenone is combined with Nebivolol.
Regorafenib Regorafenib may increase the bradycardic activities of Nebivolol.
Reserpine Reserpine may increase the hypotensive activities of Nebivolol.
Deserpidine Deserpidine may increase the hypotensive activities of Nebivolol.
Guanethidine Guanethidine may increase the hypotensive activities of Nebivolol.
Rivastigmine Nebivolol may increase the bradycardic activities of Rivastigmine.
Dabrafenib The serum concentration of Nebivolol can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Nebivolol can be increased when it is combined with Luliconazole.
Benzylpenicilloyl polylysine Nebivolol may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Spironolactone The risk or severity of hyperkalemia can be increased when Nebivolol is combined with Spironolactone.
Mirabegron The serum concentration of Nebivolol can be increased when it is combined with Mirabegron.
Nicorandil Nicorandil may increase the hypotensive activities of Nebivolol.
Molsidomine Molsidomine may increase the hypotensive activities of Nebivolol.
Insulin argine Nebivolol may increase the hypoglycemic activities of Insulin argine.
Dorzolamide Dorzolamide may increase the hypotensive activities of Nebivolol.
Bimatoprost Bimatoprost may increase the hypotensive activities of Nebivolol.
Unoprostone Nebivolol may increase the hypotensive activities of Unoprostone.
Torasemide Torasemide may increase the hypotensive activities of Nebivolol.

Target Protein

Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
Beta-3 adrenergic receptor ADRB3

Referensi & Sumber

Synthesis reference: Thomas Bader, Alfred Stutz, Harald Hofmeier, Hans-Ulrich Bichsel, "Process for preparation of racemic Nebivolol." U.S. Patent US20070149612, issued June 28, 2007.
Artikel (PubMed)
  • PMID: 16961165
    Gielen W, Cleophas TJ, Agrawal R: Nebivolol: a review of its clinical and pharmacological characteristics. Int J Clin Pharmacol Ther. 2006 Aug;44(8):344-57.
  • PMID: 1968323
    De Cree J, Cobo C, Geukens H, Verhaegen H: Comparison of the subacute hemodynamic effects of atenolol, propranolol, pindolol, and nebivolol. Angiology. 1990 Feb;41(2):95-105. doi: 10.1177/000331979004100202.
  • PMID: 2455841
    Van de Water A, Janssens W, Van Neuten J, Xhonneux R, De Cree J, Verhaegen H, Reneman RS, Janssen PA: Pharmacological and hemodynamic profile of nebivolol, a chemically novel, potent, and selective beta 1-adrenergic antagonist. J Cardiovasc Pharmacol. 1988 May;11(5):552-63. doi: 10.1097/00005344-198805000-00007.
  • PMID: 26177892
    Fongemie J, Felix-Getzik E: A Review of Nebivolol Pharmacology and Clinical Evidence. Drugs. 2015 Aug;75(12):1349-71. doi: 10.1007/s40265-015-0435-5.
  • PMID: 28509722
    Giles TD, Cockcroft JR, Pitt B, Jakate A, Wright HM: Rationale for nebivolol/valsartan combination for hypertension: review of preclinical and clinical data. J Hypertens. 2017 Sep;35(9):1758-1767. doi: 10.1097/HJH.0000000000001412.
  • PMID: 25853236
    Chen CL, Desai-Krieger D, Ortiz S, Kerolous M, Wright HM, Ghahramani P: A Single-Center, Open-Label, 3-Way Crossover Trial to Determine the Pharmacokinetic and Pharmacodynamic Interaction Between Nebivolol and Valsartan in Healthy Volunteers at Steady State. Am J Ther. 2015 Sep-Oct;22(5):e130-40. doi: 10.1097/MJT.0000000000000247.
  • PMID: 26528073
    Briciu C, Neag M, Muntean D, Bocsan C, Buzoianu A, Antonescu O, Gheldiu AM, Achim M, Popa A, Vlase L: Phenotypic differences in nebivolol metabolism and bioavailability in healthy volunteers. Clujul Med. 2015;88(2):208-13. doi: 10.15386/cjmed-395. Epub 2015 Apr 15.
  • PMID: 19561858
    Hilas O, Ezzo D: Nebivolol (bystolic), a novel Beta blocker for hypertension. P T. 2009 Apr;34(4):188-92.

Contoh Produk & Brand

Produk: 128 • International brands: 6
Produk
  • Apo-nebivolol
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Apo-nebivolol
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Apo-nebivolol
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Bystolic
    Tablet • 5 mg/1 • Oral • US • Approved
  • Bystolic
    Tablet • 10 mg/1 • Oral • US • Approved
  • Bystolic
    Tablet • 2.5 mg/1 • Oral • US • Approved
  • Bystolic
    Tablet • 5 mg/1 • Oral • US • Approved
  • Bystolic
    Tablet • 10 mg/1 • Oral • US • Approved
Menampilkan 8 dari 128 produk.
International Brands
  • Lobivon
  • Nebicard
  • Nebilet
  • Nebilong
  • Nodon
  • Nubeta

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